DE69511687T2 - Substituierte azetidinon-verbindungen als hypocholesterolemische mittel - Google Patents
Substituierte azetidinon-verbindungen als hypocholesterolemische mittelInfo
- Publication number
- DE69511687T2 DE69511687T2 DE69511687T DE69511687T DE69511687T2 DE 69511687 T2 DE69511687 T2 DE 69511687T2 DE 69511687 T DE69511687 T DE 69511687T DE 69511687 T DE69511687 T DE 69511687T DE 69511687 T2 DE69511687 T2 DE 69511687T2
- Authority
- DE
- Germany
- Prior art keywords
- aryl
- lower alkyl
- substituted
- alkyl
- coor6
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C227/00—Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C227/30—Preparation of optical isomers
- C07C227/32—Preparation of optical isomers by stereospecific synthesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/34—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
- C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
- C07C2601/14—The ring being saturated
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US21849894A | 1994-03-25 | 1994-03-25 | |
PCT/US1995/003196 WO1995026334A1 (en) | 1994-03-25 | 1995-03-22 | Substituted azetidinone compounds useful as hypocholesterolemic agents |
Publications (2)
Publication Number | Publication Date |
---|---|
DE69511687D1 DE69511687D1 (de) | 1999-09-30 |
DE69511687T2 true DE69511687T2 (de) | 2000-03-16 |
Family
ID=22815366
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
DE69511687T Expired - Lifetime DE69511687T2 (de) | 1994-03-25 | 1995-03-22 | Substituierte azetidinon-verbindungen als hypocholesterolemische mittel |
Country Status (20)
Country | Link |
---|---|
US (2) | US5627176A (de) |
EP (1) | EP0751934B1 (de) |
JP (1) | JP3524927B2 (de) |
KR (1) | KR100338171B1 (de) |
CN (1) | CN1144522A (de) |
AT (1) | ATE183738T1 (de) |
AU (1) | AU686361B2 (de) |
CA (1) | CA2186364C (de) |
CZ (1) | CZ281596A3 (de) |
DE (1) | DE69511687T2 (de) |
DK (1) | DK0751934T3 (de) |
ES (1) | ES2135050T3 (de) |
FI (1) | FI963817A0 (de) |
GR (1) | GR3031105T3 (de) |
HU (1) | HU221309B1 (de) |
NO (1) | NO964008L (de) |
NZ (1) | NZ283528A (de) |
PL (1) | PL316431A1 (de) |
SK (1) | SK119796A3 (de) |
WO (1) | WO1995026334A1 (de) |
Families Citing this family (54)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5631365A (en) | 1993-09-21 | 1997-05-20 | Schering Corporation | Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents |
US5624920A (en) * | 1994-11-18 | 1997-04-29 | Schering Corporation | Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents |
US5633246A (en) * | 1994-11-18 | 1997-05-27 | Schering Corporation | Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents |
WO1997016424A1 (en) * | 1995-11-02 | 1997-05-09 | Schering Corporation | Process for preparing 1-(4-fluorophenyl)-3(r)-(3(s)-hydroxy-3-([phenyl or 4-fluorophenyl])-propyl)-4(s)-(4-hydroxyphenyl)-2-azetidinone |
US5756470A (en) * | 1996-10-29 | 1998-05-26 | Schering Corporation | Sugar-substituted 2-azetidinones useful as hypocholesterolemic agents |
WO2000063703A1 (en) | 1999-04-16 | 2000-10-26 | Schering Corporation | Use of azetidinone compounds |
US6584357B1 (en) * | 2000-10-17 | 2003-06-24 | Sony Corporation | Method and system for forming an acoustic signal from neural timing difference data |
US6982251B2 (en) | 2000-12-20 | 2006-01-03 | Schering Corporation | Substituted 2-azetidinones useful as hypocholesterolemic agents |
SI1347987T1 (en) * | 2000-12-20 | 2005-02-28 | Schering Corporation | Sugar-substituted 2-azetidinones useful as hypocholesterolemic agents |
EP1911462A3 (de) | 2001-01-26 | 2011-11-30 | Schering Corporation | Zusammensetzungen enthaltend einen Sterolabsorptionshemmer |
BRPI0206641B8 (pt) * | 2001-01-26 | 2021-05-25 | Merck Sharp & Dohme | uso de um inibidor da absorção de esteróis |
AU2005246926B2 (en) * | 2001-01-26 | 2008-02-28 | Merck Sharp & Dohme Corp. | The use of substituted azetidinone compounds for the treatment of sitosterolemia |
US7071181B2 (en) * | 2001-01-26 | 2006-07-04 | Schering Corporation | Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors |
PL364178A1 (en) * | 2001-01-26 | 2004-12-13 | Schering Corporation | Combinations of sterol absorption inhibitor(s) with blood modifier(s) for treating vascular conditions |
SK287988B6 (sk) * | 2001-01-26 | 2012-09-03 | Schering Corporation | Composition, oral dosage form and use thereof |
CA2442219C (en) | 2001-03-28 | 2007-09-11 | Schering Corporation | Enantioselective synthesis of azetidinone intermediate compounds |
US7056906B2 (en) * | 2001-09-21 | 2006-06-06 | Schering Corporation | Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women |
JP2005504091A (ja) * | 2001-09-21 | 2005-02-10 | シェーリング コーポレイション | ステロール吸収阻害剤としてアゼチジノンを用いる黄色腫の処置 |
EP1859796A3 (de) * | 2001-09-21 | 2008-07-02 | Schering Corporation | Behandlung von xanthom mit azetidinon-derivaten als hemmer der sterol absorption |
US20030204096A1 (en) * | 2002-03-25 | 2003-10-30 | Schering Corporation | Enantioselective synthesis of azetidinone intermediate compounds |
GB0215579D0 (en) | 2002-07-05 | 2002-08-14 | Astrazeneca Ab | Chemical compounds |
US7135556B2 (en) * | 2002-07-19 | 2006-11-14 | Schering Corporation | NPC1L1 (NPC3) and methods of use thereof |
US20040132058A1 (en) | 2002-07-19 | 2004-07-08 | Schering Corporation | NPC1L1 (NPC3) and methods of use thereof |
AR040588A1 (es) * | 2002-07-26 | 2005-04-13 | Schering Corp | Formulacion farmaceutica que comprende un inhibidor de la absorcion del colesterol y un inhibidor de una hmg- co a reductasa |
CA2517571C (en) * | 2003-03-07 | 2011-07-05 | Schering Corporation | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof |
DE602004018617D1 (de) * | 2003-03-07 | 2009-02-05 | Schering Corp | Substituierte azetidinon-derivate, deren pharmazeutische formulierungen und deren verwendung zur behandlung von hypercholesterolemia |
JP2005015434A (ja) * | 2003-06-27 | 2005-01-20 | Kotobuki Seiyaku Kk | 血清コレステロール低下剤或はアテローム性硬化症の予防又は治療剤 |
US20050096307A1 (en) * | 2003-11-05 | 2005-05-05 | Schering Corporation | Combinations of lipid modulating agents and substituted azetidinones and treatments for vascular conditions |
EP1918000A2 (de) | 2003-11-05 | 2008-05-07 | Schering Corporation | Verbindungen aus lipidverändernden Wirkstoffen und substituierten Azetidinonen und Behandlungen für Gefäßzustände |
AU2004308332B2 (en) * | 2003-12-23 | 2008-04-10 | Merck Sharp & Dohme Corp. | Anti-hypercholesterolemic compounds |
CA2550215A1 (en) | 2003-12-23 | 2005-07-07 | Astrazeneca Ab | Diphenylazetidinone derivates possessing cholesterol absorption inhibitory activity |
EP1723414A4 (de) * | 2004-01-16 | 2008-03-26 | Merck & Co Inc | Npc1l1 (npc3) und verfahren zur identifizierung seiner liganden |
EP1807070A1 (de) * | 2004-09-29 | 2007-07-18 | Schering Corporation | Kombinationen aus substituierten azetidinonen und cb1-antagonisten |
CN102633730A (zh) | 2004-12-03 | 2012-08-15 | 先灵公司 | 作为cb1拮抗剂的取代哌嗪 |
WO2007001975A1 (en) * | 2005-06-20 | 2007-01-04 | Schering Corporation | Piperidine derivatives useful as histamine h3 antagonists |
SA06270191B1 (ar) | 2005-06-22 | 2010-03-29 | استرازينيكا ايه بي | مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم |
AU2007207706A1 (en) | 2006-01-18 | 2007-07-26 | Merck Sharp & Dohme Corp. | Cannibinoid receptor modulators |
WO2007100807A2 (en) | 2006-02-24 | 2007-09-07 | Schering Corporation | Npc1l1 orthologues |
CA2644905A1 (en) * | 2006-03-06 | 2007-09-13 | Teva Pharmaceutical Industries Ltd. | Ezetimibe compositions |
TW200811098A (en) | 2006-04-27 | 2008-03-01 | Astrazeneca Ab | Chemical compounds |
AU2008221833A1 (en) | 2007-03-06 | 2008-09-12 | Teijin Pharma Limited | 1-biarylazetidinone derivatives |
US20100197564A1 (en) * | 2007-04-19 | 2010-08-05 | Schering Corporation | Diaryl morpholines as cb1 modulators |
JP2010529148A (ja) * | 2007-06-07 | 2010-08-26 | テバ ファーマシューティカル インダストリーズ リミティド | エゼチミブ製造のための還元方法 |
NZ582249A (en) * | 2007-06-28 | 2012-06-29 | Intervet Int Bv | Substituted piperazines as cb1 antagonists |
US20100286160A1 (en) * | 2007-06-28 | 2010-11-11 | Intervet Inc. | Substituted piperazines as cb1 antagonists |
US20090093627A1 (en) * | 2007-08-30 | 2009-04-09 | Lorand Szabo | Process for preparing intermediates of ezetimibe by microbial reduction |
CN101200443B (zh) * | 2007-10-17 | 2011-06-29 | 中国药科大学 | 氮杂环丁酮衍生物、其制备方法及含有它们的药物组合 |
US9212175B2 (en) | 2009-03-06 | 2015-12-15 | Lipideon Biotechnology Ag | Pharmaceutical hypocholesterolemic compositions |
CN101993403B (zh) | 2009-08-11 | 2012-07-11 | 浙江海正药业股份有限公司 | 氮杂环丁酮类化合物及医药应用 |
ES2802252T3 (es) | 2012-05-01 | 2021-01-18 | Althera Life Sciences Llc | Formulación de comprimido oral que consiste en la combinación fija de rosuvastatina y ezetimiba para el tratamiento de hiperlipidemia y enfermedades cardiovasculares |
JP5969958B2 (ja) * | 2013-06-27 | 2016-08-17 | 国立大学法人お茶の水女子大学 | 光学活性含フッ素アミノ酸類の製造方法 |
CN105294426B (zh) * | 2014-06-09 | 2019-05-14 | 浙江海正药业股份有限公司 | 氮杂环丁酮化合物制备方法及其中间体 |
CN104860980B (zh) * | 2015-04-23 | 2018-06-19 | 上海弈柯莱生物医药科技有限公司 | 一种用于合成依折麦布的中间体及其制备方法和应用 |
MX2019009213A (es) | 2017-01-23 | 2019-09-27 | Dong Wha Pharm Co Ltd | Formulación compleja que comprende inhibidor de la hmg-coa reductasa y clopidogrel. |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4680391A (en) * | 1983-12-01 | 1987-07-14 | Merck & Co., Inc. | Substituted azetidinones as anti-inflammatory and antidegenerative agents |
US4803266A (en) * | 1986-10-17 | 1989-02-07 | Taisho Pharmaceutical Co., Ltd. | 3-Oxoalkylidene-2-azetidinone derivatives |
NZ228600A (en) * | 1988-04-11 | 1992-02-25 | Merck & Co Inc | 1-(benzylaminocarbonyl)-4-phenoxy-azetidin-2-one derivatives |
JPH02268144A (ja) * | 1989-04-11 | 1990-11-01 | Ube Ind Ltd | β―アミノエステルの製造法 |
US4983597A (en) * | 1989-08-31 | 1991-01-08 | Merck & Co., Inc. | Beta-lactams as anticholesterolemic agents |
US5120729A (en) * | 1990-06-20 | 1992-06-09 | Merck & Co., Inc. | Beta-lactams as antihypercholesterolemics |
ATE158789T1 (de) * | 1991-07-23 | 1997-10-15 | Schering Corp | Substituierte beta-lactam-verbindungen als hypocholesterolemische mittel und verfahren zu deren herstellung |
-
1995
- 1995-03-13 US US08/403,081 patent/US5627176A/en not_active Expired - Lifetime
- 1995-03-22 NZ NZ283528A patent/NZ283528A/en not_active IP Right Cessation
- 1995-03-22 WO PCT/US1995/003196 patent/WO1995026334A1/en active IP Right Grant
- 1995-03-22 AU AU21596/95A patent/AU686361B2/en not_active Ceased
- 1995-03-22 EP EP95914719A patent/EP0751934B1/de not_active Expired - Lifetime
- 1995-03-22 PL PL95316431A patent/PL316431A1/xx unknown
- 1995-03-22 KR KR1019960705349A patent/KR100338171B1/ko not_active IP Right Cessation
- 1995-03-22 DE DE69511687T patent/DE69511687T2/de not_active Expired - Lifetime
- 1995-03-22 CN CN95192277A patent/CN1144522A/zh active Pending
- 1995-03-22 DK DK95914719T patent/DK0751934T3/da active
- 1995-03-22 CZ CZ962815A patent/CZ281596A3/cs unknown
- 1995-03-22 ES ES95914719T patent/ES2135050T3/es not_active Expired - Lifetime
- 1995-03-22 SK SK1197-96A patent/SK119796A3/sk unknown
- 1995-03-22 CA CA002186364A patent/CA2186364C/en not_active Expired - Fee Related
- 1995-03-22 AT AT95914719T patent/ATE183738T1/de not_active IP Right Cessation
- 1995-03-22 HU HU9602616A patent/HU221309B1/hu not_active IP Right Cessation
- 1995-03-22 JP JP52518495A patent/JP3524927B2/ja not_active Expired - Fee Related
- 1995-05-18 US US08/444,167 patent/US5688990A/en not_active Expired - Lifetime
-
1996
- 1996-09-24 NO NO964008A patent/NO964008L/no unknown
- 1996-09-25 FI FI963817A patent/FI963817A0/fi unknown
-
1999
- 1999-08-27 GR GR990402188T patent/GR3031105T3/el unknown
Also Published As
Publication number | Publication date |
---|---|
JP3524927B2 (ja) | 2004-05-10 |
DE69511687D1 (de) | 1999-09-30 |
WO1995026334A1 (en) | 1995-10-05 |
AU686361B2 (en) | 1998-02-05 |
MX9604030A (es) | 1997-09-30 |
JPH09510970A (ja) | 1997-11-04 |
US5627176A (en) | 1997-05-06 |
EP0751934A1 (de) | 1997-01-08 |
ATE183738T1 (de) | 1999-09-15 |
EP0751934B1 (de) | 1999-08-25 |
CZ281596A3 (en) | 1997-05-14 |
KR970702246A (ko) | 1997-05-13 |
SK119796A3 (en) | 1997-05-07 |
GR3031105T3 (en) | 1999-12-31 |
NO964008D0 (no) | 1996-09-24 |
HU9602616D0 (en) | 1996-11-28 |
ES2135050T3 (es) | 1999-10-16 |
CA2186364A1 (en) | 1995-10-05 |
DK0751934T3 (da) | 1999-12-13 |
CA2186364C (en) | 2008-12-30 |
FI963817A (fi) | 1996-09-25 |
CN1144522A (zh) | 1997-03-05 |
HUT74887A (en) | 1997-02-28 |
AU2159695A (en) | 1995-10-17 |
NO964008L (no) | 1996-11-22 |
NZ283528A (en) | 1997-12-19 |
PL316431A1 (en) | 1997-01-06 |
HU221309B1 (en) | 2002-09-28 |
FI963817A0 (fi) | 1996-09-25 |
US5688990A (en) | 1997-11-18 |
KR100338171B1 (ko) | 2002-11-23 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
8364 | No opposition during term of opposition |